Bharti Odhav

Durban University of Technology | dut · Department of Biotechnology and Food Technology

Background and purpose: Tuberculosis has been reported to be the worldwide leading cause of death resulting from a sole infectious agent. The emergence of multidrug-resistant tuberculosis and extensively drug-resistant tuberculosis has made the battle against the infection more difficult since most currently available therapeutic options are ineff...

Novel series of diversely substituted indolizines were designed, synthesized, and evaluated for their in vitro anti-mycobacterial activity against H37Rv and multi-drug-resistant (MDR) strains of Mycobacterium tuberculosis (MTB). Many compounds exhibited significant inhibitory activity against MTB H37Rv strains. Indolizines 2d, 2e, and 4 were also f...

The cyclooxygenase-2 (COX-2) enzyme is considered to be an important target for developing novel anti-inflammatory agents. Selective COX-2 inhibitors offer the advantage of lower adverse effects that are commonly associated with non-selective COX inhibitors. In this work, a novel series of methyl 3-(substituted benzoyl)-7-substituted-2-phenylindoli...

Background: Several promising compounds against multi-drug-resistant Mycobacterium tuberculosis (MTB) are currently in the drug discovery and development pipeline. While it has yet to establish candidature in this pipeline, early results have been promising for the putative anti-mycobacterial potency of the indolizine scaffold. Methods: The molecul...

Indolizines are heteroaromatic compounds, and their synthetic analogues have reportedly showed promising pharmacological properties. In this study, a series of synthetic 7-methoxy-indolizine derivatives were synthesised, characterised and evaluated for in vitro whole-cell anti-tuberculosis (TB) screening against susceptible (H37Rv) and multi-drug-r...

Introduction The traditional method of producing instant foods involves producing a gelatinised paste from the preferred grain flour and proceeding to dry it using a drum drier. This produced a flaked product, which can be used as is or ground and sieved to obtain the desired particle size. With the advent of extrusion cooking technology and divers...

A series of methyl or ethyl 4‐(substitutedphenyl/pyridyl)‐6‐methyl‐2‐oxo/thioxo‐1,2,3,4‐tetrahydropyrimidine‐5‐carboxylate (HPM) analogues 4a‐g was synthesized and evaluated for larvicidal activity against Anopheles arabiensis. These newly synthesized compounds were characterized by spectral studies such as FT‐IR, NMR (¹H and ¹³C), LC‐MS and elemen...

Biotin is very important for the survival of Mycobacterium tuberculosis. 7,8-Diamino pelargonic acid aminotransaminase (DAPA) is a transaminase enzyme involved in the biosynthesis of biotin. The benzothiazole title compounds were investigated for their in vitro anti-tubercular activity against two tubercular strains: H37Rv (ATCC 25177) and MDR-MTB...

Five pentacyclic triterpenes were identified from the leaves and stalks of Gunnera perpensa. These were ursolic acid (I), 3-β-hydroxyolean-12-en-27-oic acid (II) (β-peltoboykinolic acid), 3-β-hydroxyurs-12-en-27-oic acid (III) (α-peltoboykinolic acid), 3-α-hydroxyolean-12-en-27-oic acid (IV), and 3α-3, 19-dihydroxyurs-12-en-28-oic acid (V) (pomolic...

A series of novel indolizine scaffold incorporating cyano group at 7 position as potential cyclooxygenase (COX)-2 inhibitors has been synthesized and characterized by FT-IR, NMR, LC-MS, and elemental analysis. Molecular modelling study was carried out to explore the COX-2 binding properties of the synthesized compounds, in an endeavour to provide a...

In the present investigation a series of novel ethyl 3-substituted-7-methylindolizine-1-carboxylates was achieved by microwave assisted one-pot method. The purity of the compounds was ascertained by HPLC and structural elucidation of the title compounds was achieved by FT-IR, NMR (¹H and ¹³C), LC-MS and elemental analysis. One randomly selected com...

Background Indolizine pharmacophore is known to exhibit various promising pharmacological properties such as analgesic, anticancer, antihistaminic, antidiabetic, anti-inflammatory, antileishmanic, antimicrobial, antimutagenic, antioxidant, antitubercular, antiviral, larvicidal and herbicidal activities. Objective In the present investigation, it w...

This study investigated the effect of processing on anti-nutritional factors of thirteen traditional leafy vegetables collected in Kwa Zulu-Natal, South Africa. The aim was to determine whether processing reduced anti-nutrient levels of leafy vegetables. The vegetables were boiled in a plant-to-distilled water ratio of 1:4 (w/v) at 97 °C for a time...

A series of trisubstituted indolizine analogues has been designed as a result of a fragment based approach to target the inhibition of mycobacterial enoyl-acyl carrier protein reductase. Anti-tuberculosis (TB) screening of the characterized compounds by a resazurin microplate assay method revealed that ethyl group at second position of indolizine n...

Design and synthesis of a new series of ethyl 7-methoxy-2-substituted-3-(substituted benzoyl) indolizine-1-carboxylates 2a-i was achieved and screened for their in vitro inhibitory activity against COX-2 enzyme. Compound 2a and 2c emerged as promising COX-2 enzyme inhibitor with IC50 of 6.56 and 6.94 µM respectively from the synthesized series when...

The new-fangled bis(4-substituted benzyl) 4-(4-substitued phenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate derivatives were synthesized by the union of substituted aryl aldehyde, tert-butyl acetoacetate, ammonium carbonate with 4-substituted benzyl alcohol via Hantzsch ester synthesis in aqueous medium under catalyst-free conditions. The...

Two recently synthesized dihydropyrimidines (DHPMs) analogues have demonstrated larvicide and repellent activity against Anopheles arabiensis. DHPMs high lipophilicity suggests that these compounds may interact directly with the membrane and modify their biophysical properties. The purpose of the present study was to characterize the interaction of...

Background: Coumarins are naturally occurring plant metabolites and several synthetic coumarin analogues are known for their various pharmacological properties such as anticoagulant, antimicrobial, anticancer, antioxidant, anti-inflammatory and antiviral properties. Objective; Keeping this promising pharmacological properties in mind, in the prese...

Buddleja saligna (family Buddlejaceae) is a medicinal plant endemic to South Africa. Two isomeric pentacyclic triterpenes, oleanolic acid and ursolic acid, were isolated from the leaves of B. saligna using silica gel column chromatography. Compounds oleanolic acid and ursolic acid were subjected to derivatization with acetic anhydride in the presen...

The title hydrate, C 13 H 14 N 2 O 4 ·H 2 O, crystallizes with two formula units in the asymmetric unit ( Z ′ = 2). The dihedral angles between the planes of the tetrahydropyrimidine ring and the 4-hydroxyphenyl ring and ester group are 86.78 (4) and 6.81 (6)°, respectively, for one molecule and 89.35 (4) and 3.02 (4)° for the other. In the crystal...

This review paper highlights current proven pharmacological research updates of Costus speciosus, a traditional medicinal herb known for many phytochemicals and ethnobotanical uses. The rhizome of these plants are used as an alternative source for diosgenin and generally used to control diabetes. Therefore, Costus speciosus is commonly called as In...

Efficient synthesis of a series of novel indolizines (2a-r) has been achieved by reaction between 4-acetyl-1-[2-(substituted phenyl)-2-oxoethyl]pyridin-1-ium bromide and substituted alkynes in presence of anhydrous potassium carbonate in dimethyl formamide medium. The title compounds have been characterized by spectroscopic techniques and elemental...

Background: Ceratotheca triloba was found to contain three anthraquinones (9, 10-anthracenedione, 1-hydroxy-4 methylanthraquinone and 5, 8-dimethoxy-2, 3, 10, 10a-tetrahydro-1H, 4aH-phenanthrene-4, 9-dione [DTP]) in its roots. Inhibition of the human topoisomerase II enzyme is the basis of some currently used cancer drugs such as doxorubicin which...

Mosquitoes are the major vectors of pathogens and parasites including those causing malaria, the most deadly vector-borne disease. The negative environmental effects of most synthetic compounds combined with widespread development of insecticide resistance encourage an interest in finding and developing alternative products against mosquitoes. In t...

Silica-sulfuric acid efficiently catalyzes conversion of aliphatic, substituted aromatic and hetero aromatic nitriles to their corresponding amides in good to excellent yields under reflux condition. Products obtained were purified by column chromatography method and characterized by ¹H NMR, ¹³C NMR and mass spectral analysis.

Six novel piperidine derivatives, compounds 5 to 10, have been synthesized and their antimicrobial and anti-oxidant activities evaluated using agar disc diffusion (antimicrobial) and 2,2-diphenyl-1- picrylhydrazyl (DPPH) scavenging capacity (antioxidant). Compound 9 revealed the least antibacterial activity. Compound 6 exhibited the strongest inhib...

Background: The traditional African herbal medicinal system has many reports of anti-diabetic food plants with no known side effects. Such plants and their products have been widely prescribed for diabetic treatment with little known mechanistic basis of their functioning. Therefore, these natural products need to be evaluated scientifically in ord...

Dihydropyrimidine scaffold has a wide range of potential pharmacological activities such as antiviral, antitubercular, antimalarial, anti-inflammatory, and anticancer properties. 5-Lipoxygenase enzyme is an enzyme responsible for the metabolism of arachidonic acid to leukotrienes. The elevated levels of this enzyme and its metabolites in cancer cel...

Mosquitoes are the major vectors of parasites and pathogens affecting humans and domestic animals. The widespread development of insecticide resistance and negative environmental effects of most synthetic compounds support an interest in finding and developing alternative products against mosquitoes. Natural coumarins and synthetic coumarin analogu...

The leaf oils of Psidium guajava (white fruit) and Psidium guajava (pink fruit) collected in KwaZulu-Natal province of South Africa has been examined by Gas chromatography-Mass spectrometry (GC-MS), and the apparent concentrations were determined by gas chromatography with a flame ionization detector. A total of twenty compounds of 88.9 % from whit...

The essential oil components of arils from seeds of Strelitzia nicolai were investigated by GC and GC-MS. The oil yields of dried arils obtained by hydrodistillation were 0.86 %. Twenty-five compounds representing 94.2 % of the S. nicolai aril oil were identified. The main chemical constituents belongs to alcohols (1.24 %), amides (3.14 %), amine (...

Abstract Traditional leafy vegetables, apart from being a staple in the diet of most of sub-Saharan Africa, are an essential part of traditional medicine and are used daily by traditional healers in the region to treat a wide variety of ailments. In this study, a batch culture technique was used to investigate whether 25 infusions from 22 tradition...

A new polymorph belonging to the tetrahydropyrimidinium class of compounds, namely 6-(4-chlorophenyl)-5-(methoxycarbonyl)-4-methyl-2-(3-(trifluoromethylthio)phenylamino)-3,6-dihydropyrimidin-1-ium chloride, and a hydrate of 2-(3-bromophenylamino)-6-(4-chlorophenyl)-5-(methoxycarbonyl)-4-methyl-3,6-dihydropyrimidin-1-ium chloride, have been isolated...

The determination of the crystal and molecular structure of organic compounds has contributed immensely towards the area of crystal engineering. This contributes towards the understanding of the molecular geometry and the different intermolecular interactions which control crystal packing. An approach which quantifies the energetics associated with...

The objective of this experiment was to assess the effects of malting, extrusion and a combination of both processes on the physical and functional properties of the pearl millet flour (PMF) and pearl millet based instant beverage powder (PMIBP) produced. PMF and PMIBP were prepared by malting, extrusion and a combination of malting and extrusion c...

Eight novel dihydropyrimidine analogs named DHPM1-DHPM8 was synthesized in their hydrochloride salt form using one pot synthesis between methyl 2-chloro-4-(4-chlorophenyl)-6-methyl-1,4-dihydropyrimidine-5-carboxylate and substituted arylamines in isopropanol. The antimosquito effect of the test compounds were assessed against the adult mosquito Ano...

Photodynamic therapy (PDT) is an emerging medical treatment that uses photosensitizers (drug) which are activated by laser light for the generation of cytotoxic free radicals and singlet oxygen molecules that cause tumor cell death. In the recent years, there has been a focus on using and improving an industrial colorant termed phthalocyanines as a...

Dihydropyrimidine scaffold has a wide range of potential pharmacological activities such as antiviral, antitubercular, antimalarial, anti-inflammatory, and anticancer properties. 5-Lipoxygenase enzyme is an enzyme responsible for the metabolism of arachidonic acid to leukotrienes. The elevated levels of this enzyme and its metabolites in cancer cel...

Dihydropyrimidine scaffold has a wide range of potential pharmacological activities such as antiviral, antitubercular, antimalarial, anti-inflammatory, and anticancer properties. 5-Lipoxygenase enzyme is an enzyme responsible for the metabolism of arachidonic acid to leukotrienes. The elevated levels of this enzyme and its metabolites in cancer cel...

Pathogens frequently display resistance to current drugs, which frequently lack selectivity/efficacy and have detrimental side effects. Thus, there is a constant need for novel therapeutic agents. Coumarins belong to the family of lactones, having a benzopyrone system that can be isolated from plants as well as total synthesis that can be carried o...

Seed dormancy depends on biotic and abiotic factors and one of the important factors is seed germination. Some live seeds are dormant and need more time, and/or need to be subjected to specific environmental conditions before they will germinate and other seeds are recalcitrant seeds that cannot be stored as they germinate rapidly due to their high...

In the present work, we demonstrated a simple and an efficient method for the condensation of substituted aryl/heteroaryl amines with acetonylacetone in the presence of trifluoro acetic acid to afford the corresponding 2,5-dimethyl-1-substitued pyrroles using Paal-Knorr synthesis in excellent yields. Trifluoroacetic acid was used under reflux condi...

Metal-based phthalocyanines currently are utilized as a colorant for industrial applications but their unique properties also make them prospective photosensitizers. Photosensitizers are non-toxic drugs, which are commonly used in photodynamic therapy (PDT), for the treatment of various cancers. PDT is based on the principle that, exposure to light...

In the title compound, C21H13Cl2NO2S, the benzo­thia­zole ring makes dihedral angles of 0.94 (1) and 70.65 (5)° with the 4-chloro­phenyl­methanone unit and the 5-chloro­phenyl ring, respectively. The dihedral angle between the 4-chloro­phenyl­methanone unit and the 5-chloro­phenyl ring is 66.20 (5)°. The crystal structure consists of dimeric units...

In the title compound, C21H14BrNO2S, the dihedral angle between the planes of the benzo-thia-zole and phenyl-methanone groups is 63.4 (2)°. In the crystal, pairs of C-H⋯N hydrogen bonds link the mol-ecules to form inversion dimers, which are further linked by C-H⋯O inter-actions into chains along the c axis. C-H⋯π and π-π inter-actions [centroid-ce...

a b s t r a c t A novel and efficient one pot synthesis was developed for 2,6-substituted-benzo[d]thiazole analogues 4a ek and 2,4-substituted-benzo[d]thiazole analogues 4lep via three component condensation reaction of substituted arylaldehyde, 2-amino-6-halo/4-methyl-benzo[d]thiazole and 2-naphthol or 6-hydroxy quinoline in presence of 10% w/v Na...

Coumarin (2H-1-benzopyran-2-one) is a plant-derived natural product known for its pharmacological properties such as anti-inflammatory, anticoagulant, antibacterial, antifungal, antiviral, anticancer, antihypertensive, antitubercular, anticonvulsant, antiadipogenic, antihyperglycemic, antioxidant, and neuroprotective properties. Dietary exposure to...

A novel and efficient one pot synthesis was developed for 2,6-substituted-benzo[d]thiazole analogues 4a-k and 2,4-substituted-benzo[d]thiazole analogues 4l-pvia three component condensation reaction of substituted arylaldehyde, 2-amino-6-halo/4-methyl-benzo[d]thiazole and 2-naphthol or 6-hydroxyquinoline in presence of 10% w/v NaCl in water by micr...

The anti-bacterial and anti-fungal activity of four aqueous plant extracts (1 x 10 4 μg/ml) of 2,3'4,5'-tetra hydroxy-4'-geranylstilbene (chlorophorin) and 3',4, 5' - trihydroxy - 4' - geranylstilbene (Iroko) from the tree Chlorophora excelsa and (6aR,11aR)-3-hydroxy-8,9-methylenedioxypterocarpan (Maackiain) and 7-hydroxy-4'-methoxyisoflavone (form...

9, 10-Anthracenedione and 1-hydroxy-4-methylanthraquinone showed antibacterial activity against Staphylococcus aureus, Micrococcus luteus, Bacillus cereus and Escherichia coli. Due to the synergistic effect of the individual compounds, the crude extract from leaves and roots of Ceratotheca triloba exhibited good potency (>500) against S. aureus and...

In the title molecular salt, C19H18BrClN3O2 +·Cl−, the dihedral angles between the pyrimidine ring and the chlorobenzene and bromobenzene rings are 72.4 (2) and 45.5 (2)°, respectively. The dihedral angle between the chlorobenzene and bromobenzene rings is 27.5 (2)°. The conformation of the mol­ecule is stabilized by an intra­molecular C—H⋯O inter­...

Traditionally, leaf infusions of Brachylaena discolor are used for the treatment of diabetes and renal conditions. Therefore, the aim of this study was to evaluate the effect of a methanolic leaf extract of B. discolor in a streptozotocin (STZ)-induced diabetic rat model. Diabetes was induced in Wistar rats by an intraperitoneal injection of STZ; b...

Coumarin (2H-1-benzopyran-2-one) is a plant-derived natural product known for its pharmacological properties such as anti-inflammatory, anticoagulant, antibacterial, antifungal, antiviral, anticancer, antihypertensive, antitubercular, anticonvulsant, antiadipogenic, antihyperglycemic, antioxidant, and neuroprotective properties. Dietary exposure to...